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19 results on '"Salman Y"'

10. Highly regioselective ring opening of quinolinic[2,3]anhydrides under mild conditions

Author

Choung U. Kim, Sammy Metobo, Haolun Jin, Salman Y. Jabri, Jared W. Evans, and Evangelos Aktoudianakis

Subjects
Organic Chemistry, chemistry.chemical_element, Regioselectivity, Ring (chemistry), Biochemistry, Medicinal chemistry, Lewis acid catalysis, chemistry, Drug Discovery, Lanthanum, Lewis acids and bases, Trifluoromethanesulfonate, Stoichiometry, Indium
Abstract

We report a study of the influence of Lewis acids upon the regioselectivity of ring opening of quinolinic[2,3]anhydrides to provide 2-(isopropoxycarbonyl)-nicotinic acids. In the presence of stoichiometric amounts of indium trifluoromethanesulfonate or lanthanum trifluoromethanesulfonate, the desired 2-position ester was generated with greater than 95:5 regioselectivity. This methodology was also applied to 6-methyl-[2,3]-quinoline to provide similar results.

Published
2013
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11. Tricyclic HIV integrase inhibitors: VI. SAR studies of ‘benzyl flipped’ C3-substituted pyrroloquinolines

Author

Manuel Tsiang, Matthew R. Wright, Choung U. Kim, Salman Y. Jabri, Sammy Metobo, Haolun Jin, Xiaowu Chen, Mish Michael R, and Rachael A. Lansdown

Subjects
Anti-HIV Agents, Stereochemistry, Clinical Biochemistry, Human immunodeficiency virus (HIV), Administration, Oral, Pharmaceutical Science, medicine.disease_cause, Biochemistry, Structure-Activity Relationship, chemistry.chemical_compound, Dogs, Drug Discovery, medicine, Animals, Humans, Potency, Pyrroles, HIV Integrase Inhibitors, Molecular Biology, chemistry.chemical_classification, Molecular Structure, Organic Chemistry, Rats, chemistry, Drug Design, Quinolines, Lactam, Molecular Medicine, Tricyclic
Abstract

A series of C3 halobenzyl-substituted tricyclic HIV integrase inhibitors was prepared. Improvement in cell-based inhibitor potency was observed in comparison to previously disclosed tricyclic pyrroloquinolines carrying the ‘halobenzyl tail’ at the lactam nitrogen. Animal PK for several of the C3-substituted inhibitors was examined, with a dihaloaryl analog achieving good balance in protein-shifted EC50 and t1/2 in animal PK studies.

Published
2009
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12. Tricyclic HIV integrase inhibitors: Potent and orally bioavailable C5-aza analogs

Author

Choung U. Kim, Richard W. Pastor, Matthew R. Wright, Haolun Jin, Salman Y. Jabri, Peter Pyun, Sammy Metobo, Rachael A. Lansdown, Manuel Tsiang, Ruby Cai, Xiaowu Chen, and Mish Michael R

Subjects
Stereochemistry, Clinical Biochemistry, Administration, Oral, Biological Availability, Pharmaceutical Science, Integrase inhibitor, Crystallography, X-Ray, Biochemistry, Dogs, Oral administration, Raltegravir Potassium, Drug Discovery, medicine, Animals, Humans, HIV Integrase Inhibitors, Organic Chemicals, Molecular Biology, chemistry.chemical_classification, biology, Organic Chemistry, Sulfonamide (medicine), biology.organism_classification, Pyrrolidinones, Rats, Integrase, stomatognathic diseases, Enzyme, chemistry, Enzyme inhibitor, Lentivirus, Azacitidine, biology.protein, Molecular Medicine, Tricyclic, medicine.drug
Abstract

A series of C5-aza tricyclic HIV integrase inhibitors was prepared. A highly potent and orally bioavailable compound (compound 9) was identified and selected for development.

Published
2008
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